FI96691B - Förfarande för framställning av nya terapeutiskt användbara /1,4/oxazino/3,4-a//2/bensazepinderivat - Google Patents

Förfarande för framställning av nya terapeutiskt användbara /1,4/oxazino/3,4-a//2/bensazepinderivat Download PDF

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Publication number
FI96691B
FI96691B FI943363A FI943363A FI96691B FI 96691 B FI96691 B FI 96691B FI 943363 A FI943363 A FI 943363A FI 943363 A FI943363 A FI 943363A FI 96691 B FI96691 B FI 96691B
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Finland
Prior art keywords
oxo
formula
oxazino
compound
phenylpropyl
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FI943363A
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English (en)
Finnish (fi)
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FI943363A0 (sv
FI96691C (sv
FI943363A (sv
Inventor
Timothy Paul Burkholder
Gary Alan Flynn
Douglas Wade Beight
Philippe Bey
Alan M Warshawsky
Shujaath Mehdi
Eugene Lewis Giroux
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Merrell Dow Pharma
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Publication of FI943363A0 publication Critical patent/FI943363A0/sv
Publication of FI943363A publication Critical patent/FI943363A/sv
Publication of FI96691B publication Critical patent/FI96691B/sv
Application granted granted Critical
Publication of FI96691C publication Critical patent/FI96691C/sv

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (3)

1. Förfarande för framställning av nya terapeutiskt användbara [1,4]oxazino[3,4-a][2]bensazepinderivat med 5 formeln H H \ J H 10 (11) S //^ N \ ° )—° ^ch^s-r3 coor4 r2 15 där R2 är bensyl; R3 är väte eller acetyl; och R4 är väte, metyl, difenylmetyl eller pivaloyloximetyl; kännetecknat därav, att 20 a) för framställning av förenlngar med formeln II, där R3 är acetyl och R4 är difenylmetyl; omsätts en före-nlng med formeln
25 H * ,J \ H (III) h2n °^!L/0
30 COOR4 där R4 är difenylmetyl, med en förening med formeln H 5R3 24 96691 där R3 är acetyl och R2 är bensyl, 1 närvaro av ett kopp-lingsmedel, eller b) för frainställnlng av förenlngar med formeln II, där R3 är acetyl och R4 är väte; omsätts en förenlng med 5 formeln \ .JD ίο jh**' \ (iv) 1 0 ch^s-r3 coor4 / R2 15 där R2 är bensyl, R3 är acetyl och R4 är difenylmetyl, med en syra, eller c) för framställning av förenlngar med formeln II, där R3 är väte och R4 är väte; omsätts en förenlng med for- 20 meln \ 25 0;5::Γ^ N ^ \ (V) 0 CH^S-R3 COOR4 / R2 30 där R2 och R4 betecknar samma som ovan, och R3 är acetyl, med en bas, eller d) för framställning av förenlngar med formeln II, där R3 är acetyl och R4 är metyl, difenylmetyl eller piva- 35 loyloximetyl; omsätts en förenlng med formeln il 14 t 4ll« l i t #* : : 25 96691 \ -rO \ J I H 5 °Yb^ ° X-y ch^s-r3 coor4 / R2 10 där R2 är bensyl, R3 är acetyl och R4 är väte, i närvaro av en bas med en lämplig metylhalogenid, klormetylplvalat eller difenylmetylhalogenid.
2. Förfarande enligt patentkravet 1, känne- t e c k n a t därav, att man framställer [4s-[4a,7a(R*),-15 12bp] ] —7— [ (l-oxo-2(s)-tio-3-fenylpropyl)amino] -1,2,3,4,- 6,7,8,12b-hexahydro-6-oxo-lH-[l,4]-oxazino[3,4-a][2]-bensazepln-4-karboxylsyra.
3. Förfarande enligt patentkravet 1, känne- t e c k n a t därav, att man framställer [4s-[4a,7a(R*),~ 20 12bp] ] -7- [ (l-oxo-2( s )-acetyltio-3-fenylpropyl )amino] -1,2,- 3,4,6,7,8,12b-hexahydro-6-oxo-lH-[l,4]-oxazino[3,4-a][2]-bensazepin-4-karboxylsyra. ♦ « 4
FI943363A 1990-10-18 1994-07-14 Förfarande för framställning av nya terapeutiskt användbara /1,4/oxazino/3,4-a//2/bensazepinderivat FI96691C (sv)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US60005290A 1990-10-18 1990-10-18
US60005290 1990-10-18
US73549691A 1991-07-25 1991-07-25
US73549691 1991-07-25

Publications (4)

Publication Number Publication Date
FI943363A0 FI943363A0 (sv) 1994-07-14
FI943363A FI943363A (sv) 1994-07-14
FI96691B true FI96691B (sv) 1996-04-30
FI96691C FI96691C (sv) 1996-08-12

Family

ID=27083513

Family Applications (2)

Application Number Title Priority Date Filing Date
FI914905A FI95255C (sv) 1990-10-18 1991-10-17 Förfarande för framställning av nya terapeutiskt användbara merkaptoacetylamidopyrrolo- och -pyridobensazepinderivat
FI943363A FI96691C (sv) 1990-10-18 1994-07-14 Förfarande för framställning av nya terapeutiskt användbara /1,4/oxazino/3,4-a//2/bensazepinderivat

Family Applications Before (1)

Application Number Title Priority Date Filing Date
FI914905A FI95255C (sv) 1990-10-18 1991-10-17 Förfarande för framställning av nya terapeutiskt användbara merkaptoacetylamidopyrrolo- och -pyridobensazepinderivat

Country Status (18)

Country Link
EP (1) EP0481522B1 (sv)
JP (1) JP3181335B2 (sv)
KR (1) KR100372491B1 (sv)
CN (2) CN1036590C (sv)
AT (1) ATE161536T1 (sv)
AU (1) AU642535B2 (sv)
CA (1) CA2053340C (sv)
DE (1) DE69128516T2 (sv)
DK (1) DK0481522T3 (sv)
ES (1) ES2114870T3 (sv)
FI (2) FI95255C (sv)
GR (1) GR3026222T3 (sv)
HU (1) HU210008B (sv)
IE (1) IE913648A1 (sv)
IL (1) IL99769A (sv)
NO (1) NO180718C (sv)
NZ (1) NZ240230A (sv)
PT (1) PT99267B (sv)

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ZA874106B (en) * 1986-06-13 1987-12-08 Merrell Dow Pharmaceuticals Inc. Novel antihypertensive agent
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DE69128516T2 (de) 1998-07-23
PT99267A (pt) 1992-08-31
PT99267B (pt) 1999-04-30
CN1058013C (zh) 2000-11-01
FI943363A0 (sv) 1994-07-14
JP3181335B2 (ja) 2001-07-03
GR3026222T3 (en) 1998-05-29
AU8581991A (en) 1992-04-30
NO180718C (no) 1997-06-04
KR920008040A (ko) 1992-05-27
FI914905A (sv) 1992-04-19
NO914092L (no) 1992-04-21
ATE161536T1 (de) 1998-01-15
CA2053340C (en) 2002-04-02
KR100372491B1 (ko) 2003-05-27
FI95255C (sv) 1996-01-10
FI96691C (sv) 1996-08-12
DE69128516D1 (de) 1998-02-05
CN1166490A (zh) 1997-12-03
HU913282D0 (en) 1992-01-28
DK0481522T3 (da) 1998-03-09
JPH04282382A (ja) 1992-10-07
CN1061971A (zh) 1992-06-17
FI943363A (sv) 1994-07-14
IL99769A (en) 1998-12-27
EP0481522B1 (en) 1997-12-29
IE913648A1 (en) 1992-04-22
FI914905A0 (sv) 1991-10-17
NZ240230A (en) 1993-01-27
CN1036590C (zh) 1997-12-03
NO914092D0 (no) 1991-10-17
IL99769A0 (en) 1992-08-18
ES2114870T3 (es) 1998-06-16
NO180718B (no) 1997-02-24
HUT63419A (en) 1993-08-30
EP0481522A1 (en) 1992-04-22
CA2053340A1 (en) 1992-04-19
HU210008B (en) 1995-01-30
FI95255B (sv) 1995-09-29
AU642535B2 (en) 1993-10-21

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